PI-103

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本试剂(PI-103)
仅供科研实验使用,不得用于其他用途！

简介：
货 号：P-9099
名 称：PI-103
别 名：PI-103 Free Base
C A S ：371935-74-9
分子量：348.36
分子式：C19H16N4O3
纯 度：HPLC/TLC:>99%
说 明：Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO. Disposal: A
文 献：PI-103 is a potent and selective PI3K inhibitor with low IC50 values against PI3K isoforms p110α (2 nM), p110β (3 nM), p110δ (3 nM), and p110γ (15 nM). PI-103 at 0.5 µM also inhibited TORC1 by 84% and demonstrated an IC50 of 14 nM against DNA-PK. PI-103 potently inhibited proliferation and invasion of a wide variety of human cancer cells in vitro and induced tumor growth delay in eight different human cancer xenograft models. PI-103 also demonstrated antiangiogenic potential. Raynaud F.I., et al. "Pharmacologic characterization of a potent inhibitor of class I phosphatidylinositide 3-kinases." Cancer Res. 67: 5840-5850 (2007). PI-103 had antitumor activity in two gefitinib-resistant (please see Cat. No. G-4408, Gefitinib, Free Base) non-small cell lung cancer cell lines, A549 and H460, possibly by simultaneously inhibiting p70s6k phosporylation and Akt phosphorylation due to mTOR inhibition. Zou Z.Q., et al. "A novel dual PI3Kalpha/mTOR inhibitor PI-103 with high antitumor activity in non-small cell lung cancer cells." Int. J. Mol. Med. 24: 97-101 (2009). PI-103 was mainly cytostatic for human leukemic cell lines and induced cell cycle arrest in the G1 phase. In blast cells from AML patients, PI-103 inhibited leukemic proliferation and the clonogenicity of leukemic progenitors, and induced mitochondrial apoptosis. Park S., et al. "PI-103, a dual inhibitor of Class IA phosphatidylinositide 3-kinase and mTOR, has antileukemic activity in AML." Leukemia 22: 1698-1706 (2008). PI-103 inhibited the proliferation of glioma cells, possibly by its ability to inhibit both PI3 kinaseα and mTOR. It showed significant inhibitory activity in xenografted tumors with no observable toxicity. Fan Q.W., et al. "A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma." Cancer Cell 9: 341-349 (2006). A combined treatment with arsenic disulfide and PI-103 synergistically killed non-acute promyelocytic leukemia cells and promoted their differentiation in vitro. Hong Z., et al. "Arsenic disulfide synergizes with the phosphoinositide 3-kinase inhibitor PI-103 to eradicate acute myeloid leukemia stem cells by inducing differentiation." Carcinogenesis 32: 1550-1558 (2011). PI-103 inhibited endothelial cell proliferation and survival in vitro and tumor growth in vivo possibly by blocking activation of both PI3K and mTOR in vGPCR-expressing endothelial cells. Chaisuparat R., et al. "Dual inhibition of PI3Kα and mTOR as an alternative treatment for Kaposi's sarcoma." Cancer Res. 68: 8361-8368 (2008).